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1. 发明申请

WO1995024399A1 5-HT3 RECEPTOR AGONIST, NOVEL THIAZOLE DERIVATIVE, AND INTERMEDIATE THEREFOR 审中-公开
标题翻译： 5-HT3受体激动剂，新型噻唑衍生物及其中间体
公开(公告)号：WO1995024399A1
公开(公告)日：1995-09-14
申请号：PCT/JP1995000385
申请日：1995-03-09
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , IWAOKA, Kiyoshi , ANAN, Hideki , IMANISHI, Naoki , KAZUTA, Kenichi , KOSHIO, Hiroyuki , SUZUKI, Takeshi , ITAHANA, Hirotsune , ITO, Hiroyuki , MIYATA, Keiji , OHTA, Mitsuaki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/28
CPC分类号： C07D277/60 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D513/04 , Y02P20/55
摘要： A 5-HT3 receptor agonist containing a thiazole derivative represented by general formula (I) as the active ingredient, a specified compound useful as a 5-HT3 receptor agonist, and a specified thioamide derivative useful as an intermediate therefor, wherein ring A represents one of the following rings which may be substituted by at least one substituent selected from the group consisting of halogen, lower alkyl and lower alkoxy: (1) a benzene ring, and (2) a 5- or 6-membered unsaturated heterocycle having one or two heteroatoms selected from among nitrogen, oxygen and sulfur; one of L and L represents a single bond, and the other of them is absent, or represents C1-C4 alkylene or C2-C5 alkenylene; R represents a group represented by any of general formulae: (1), (2), (3) and (4); L represents lower alkylene; L represents a single bond or lower alkylene; R and R represent each independently hydrogen, lower alkyl or an amino-protecting group; R represents hydrogen, lower alkyl, oxo or optionally protected amino; R is absent, or represents hydrogen, lower alkyl, aralkyl or an amino-protecting group; ring B represents one of the following rings which are either monocyclic or bicyclic and may bear an oxygen atom(s): (1) a nitrogenous saturated heterocycle bearing four to sixteen ring atoms, and (2) a nitrogenous heterocycle having a double bond and bearing four to sixteen ring atoms: and ring D represents a saturated carbocycle bearing four to eight ring atoms; provided the nitrogen atom of R may form an unsubstituted quaternary ammonium salt.
摘要翻译：含有由通式（I）表示的噻唑衍生物作为活性成分的5-HT 3受体激动剂，可用作5-HT 3受体激动剂的特定化合物和用作其中间体的特定硫代酰胺衍生物，其中环A表示1 可以被选自卤素，低级烷基和低级烷氧基的至少一个取代基取代的以下环：（1）苯环，和（2）具有一个或多个的一个或多个的5-或6-元不饱和杂环，选自氮，氧和硫的两个杂原子; L 1和L 2之一表示单键，另一个不存在，或表示C1-C4亚烷基或C2-C5亚烯基; R表示由通式（1），（2），（3）和（4）中的任一个表示的基团。 L 3表示低级亚烷基; L 4代表单键或低级亚烷基; R 1和R 2各自独立地表示氢，低级烷基或氨基保护基; R 3表示氢，低级烷基，氧代或任选保护的氨基; R 4不存在，或表示氢，低级烷基，芳烷基或氨基保护基; 环B表示单环或双环的以下环之一，并且可以带有氧原子：（1）具有4至16个环原子的含氮饱和杂环，和（2）具有双键的含氮杂环和具有四至十六个环原子：环D表示带有四至八个环原子的饱和碳环; 条件是R的氮原子可以形成未取代的季铵盐。

2. 发明申请

WO1995024406A1 NOVEL 2-(IMIDAZOLYLMETHYL)THIAZOLE DERIVATIVE AND MEDICINAL COMP OSITION THEREOF 审中-公开
标题翻译：新的2-（咪唑烷基）噻唑衍生物及其药物组合物
公开(公告)号：WO1995024406A1
公开(公告)日：1995-09-14
申请号：PCT/JP1995000386
申请日：1995-03-09
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , IWAOKA, Kiyoshi , KAZUTA, Kenichi , NAGASHIMA, Shinya , ITO, Hiroyuki , MIYATA, Keiji , OHTA, Mitsuaki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： A 2-(imidazolylmethyl)thiazole derivative represented by general formula (I) and useful as a 5-HT3 receptor agonist, a salt thereof, and a medicinal composition thereof, wherein Het represents (a) a five-membered unsaturated heterocyclic group which contains at least one atom selected from among nitrogen, oxygen and sulfur and may be substituted, or (b) a benzofuran or benzothiophene ring group; and R represents hydrogen, lower alkyl, lower alkenyl, cycloalkyl, halogenated lower alkyl, optionally substituted aryl or optionally substituted aralkyl.
摘要翻译：由通式（I）表示的可用作5-HT 3受体激动剂的2-（咪唑基甲基）噻唑衍生物及其药物组合物及其药物组合物，其中Het表示（a）五元不饱和杂环基，其含有至少一个选自氮，氧和硫的原子，可被取代，或（b）苯并呋喃或苯并噻吩环基团; R代表氢，低级烷基，低级烯基，环烷基，卤代低级烷基，任意取代的芳基或任意取代的芳烷基。

3. 发明申请

WO1995018121A1 NOVEL BENZYLAMINE DERIVATIVE 审中-公开
标题翻译：新型苯甲酰胺衍生物
公开(公告)号：WO1995018121A1
公开(公告)日：1995-07-06
申请号：PCT/JP1994002164
申请日：1994-12-21
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , SUGA, Akira , KAZUTA, Kenichi , MORIHIRA, Koichiro , MATSUDA, Koyo , KAKUTA, Hirotoshi , MORITANI, Hiroshi , IIZUMI, Yuichi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D333/20
CPC分类号： C07D409/14 , C07D333/16 , C07D333/20 , C07D409/04 , C07D409/12 , C07D417/04
摘要： A benzylamine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having a potent squalene epoxidase inhibitory activity without being accompanied by adverse effects and thus being usable as a suitable cholesterol-lowering drug. In said formula, ring A represents a benzene ring or an unsaturated 5- or 6-membered heterocycle having one to three heteroatoms of one or more kinds selected from the group consisting of oxygen, sulfur and nitrogen; R represents lower alkyl; ring B represents an aromatic carbocycle or unsaturated 5- or 6-membered heterocycle having one or two heteroatoms of one or two kinds selected from the group consisting of sulfur and nitrogen; and R and R represent each independently hydrogen, halogen, hydroxy, lower alkoxy, lower alkanoyl, lower alkoxycarbonyl, cyano, nitro, amino, dioxolanyl, or lower alkyl which may be substituted by halogen, hydroxy or amino.
摘要翻译：由通式（I）表示的苄胺衍生物或其药学上可接受的盐，具有强效的角鲨烯环氧酶抑制活性，不伴随不良反应，因此可用作合适的降胆固醇药物。在所述式中，环A表示具有1至3个选自氧，硫和氮的一种或多种的一种或多种杂原子的苯环或不饱和5-或6-元杂环; R 1表示低级烷基; 环B表示具有一个或两个选自硫和氮的一种或两种的杂原子的芳族碳环或不饱和5-或6-元杂环; R 2和R 3各自独立地表示可被卤素，羟基或氨基取代的氢，卤素，羟基，低级烷氧基，低级烷酰基，低级烷氧基羰基，氰基，硝基，氨基，二氧戊环基或低级烷基。

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